Synthesis of new verapamil analogues and their evaluation in combination with rifampicin against Mycobacterium tuberculosis and molecular docking studies in the …

…, E Pavadai, K Naran, DF Warner, PG Ruminski…

Index: Singh, Kawaljit; Kumar, Malkeet; Pavadai, Elumalai; Naran, Krupa; Warner, Digby F.; Ruminski, Peter G.; Chibale, Kelly Bioorganic and Medicinal Chemistry Letters, 2014 , vol. 24, # 14 p. 2985 - 2990

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Citation Number: 8

Abstract

Abstract New verapamil analogues were synthesized and their inhibitory activities against Mycobacterium tuberculosis H37Rv determined in vitro alone and in combination with rifampicin (RIF). Some analogues showed comparable activity to verapamil and exhibited better synergies with RIF. Molecular docking studies of the binding sites of Rv1258c, a M. tuberculosis efflux protein previously implicated in intrinsic resistance to RIF, suggested a ...